Synthesis of novel and potent vorapaxar analogues†
Vorapaxar is a first-in-class PAR-1 antagonistic drug based on the ent-himbacine scaffold. Detailed in this article are enantioselective and racemic routes to various novel vorapaxar analogues. Biological testing revealed these compounds to have moderate to excellent potencies against PAR-1 with the most potent analogue demonstrating an IC50 of 27 nM.
- This article is part of the themed collection: Contemporary Synthetic Chemistry in Drug Discovery